title: Reproducibility of post-amphetamine [11C]FLB 457 binding to cortical D2/3 receptors.
abstract: In a recent positron emission tomography (PET) study, we demonstrated the ability to measure amphetamine-induced dopamine (DA) release in the human cortex with the relatively high affinity dopamine D2/3 radioligand [(11)C]FLB 457. Herein we report on reproducibility and reliability of [(11)C]FLB 457 binding potential relative to non-displaceable uptake (BP(ND)) following an acute amphetamine challenge. Ten healthy human subjects were studied twice with [(11)C]FLB 457 following an acute amphetamine (oral, 0.5 mg kg(-1) dose) challenge on two-separate days approximately one week apart. D2/3 receptor binding parameters were estimated using a two-tissue compartment kinetic analysis in the cortical regions of interest and cerebellum (reference region). The test-retest variability and intraclass correlation coefficient were assessed for distribution volume (V(T)), binding potential relative to plasma concentration (BP(P)), and BP(ND) of [(11)C]FLB 457. The test-retest variability of [(11)C]FLB 457 V(T), BP(P) and BP(ND) were ≤ 17%, 22% and 11% respectively. These results, which are consistent with the published test-retest variability for this ligand measured under baseline conditions demonstrate that the post-amphetamine [(11)C]FLB 457 BP(ND) is reproducible. These data further support the use [(11)C]FLB 457 and amphetamine to characterize cortical dopamine transmission in neuropsychiatric disorders.
authors.affiliation: Department of Radiology, University of Pittsburgh, Pittsburgh, Pennsylvania, United States of America.
authors.forename: Rajesh
authors.initials: R
authors.lastname: Narendran
authors.forename: Michael
authors.initials: M
authors.lastname: Himes
authors.forename: N Scott
authors.initials: NS
authors.lastname: Mason
mesh_terms: D000661:Amphetamine / Q000008:administration & dosage / Q000494:pharmacology*; D002250:Carbon Radioisotopes / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism*; D018492:Dopamine Antagonists / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008279:Magnetic Resonance Imaging; D049268:Positron-Emission Tomography; D011759:Pyrrolidines / Q000378:metabolism*; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050637:Receptors, Dopamine D3 / Q000378:metabolism*; D015203:Reproducibility of Results; D012457:Salicylamides / Q000378:metabolism*
chemical_list: D002250:Carbon Radioisotopes; D018492:Dopamine Antagonists; D011759:Pyrrolidines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D012457:Salicylamides; C065065:FLB 457; D000661:Amphetamine; D004298:Dopamine